化合物 SB-505124|T2462|TargetMol

SB-505124
694433-59-5

￥258 1mg 起订

￥367 2mg 起订

￥576 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 SB-505124

英文名称：: SB-505124

CAS号：: 694433-59-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.92%

产品类别：: 抑制剂

货号：: T2462

Product Introduction

Bioactivity

名称	SB-505124
描述	SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
细胞实验	Cell viability is measured as described by Laping et al., 2002 or by using the modified tetrazolium salt WST-1. XTT assay: The cells are serum-deprived for 24 hours and then treated with SB505124 for 48 hours to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 hours with XTT labeling and electron coupling reagent according to the manufacturer's directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells. Modified tetrazolium salt WST-1: Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB505124 (to achieve the final concentrations indicated) for 30 minutes before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 hours at 37 °C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate.(Only for Reference)
激酶实验	In Vitro Protein Kinase Assay : Kinase assays are performed as described by Laping et al., 2002 using the kinase domain of ALK5 and full-length N-terminal fused GST-Smad3. Kinase assays are performed with 65 nM GST-ALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 μM ATP. Reactions are incubated with 0.5 μCi of [33P]γATP for 3 hours at 30 °C. Phosphorylated protein is captured on P-81 paper , washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein is also coated onto FlashPlate Sterile Basic Microplates. Kinase assays are then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates are washed three times with phosphate buffer and counted by TopCount.
体外活性	在兔GFS模型中,SB505124降低了GFS手术部位的眼内压（IOP）水平并减少了结膜下细胞浸润和瘢痕形成.在他克莫司（TAC）治疗的小鼠和FK12EC KO小鼠中,SB505124抑制内皮细胞TGF-β受体的活化和肾小动脉玻璃样变性的诱导.
体内活性	SB505124被鉴定为ALK4和ALK5的可逆ATP竞争性和选择性ALK抑制剂。SB-505124抑制紧密相关的ALK4,IC50为129 nM,选择性比作用于ALK5低2.5倍。SB-505124浓度高达10 μM时也不抑制ALK2。SB-505124抑制COS-1细胞内源性Smad2磷酸化。ALK4和ALK5激活Smad1和Smad2,加入SB-505124抑制激活。SB-505124作用于HepG2人类肝癌细胞,C2C12小鼠成肌细胞和Mv1Lu水貂肺细胞,浓度依赖性抑制转化生长因子-β诱导的Smad2磷酸化。SB-505124有效抑制转化生长因子-β和活化素诱导CAGA12-荧光素酶和ARE-荧光素酶受体结构的活力,这种作用存在浓度依赖性。在人脐静脉内皮细胞（HUVEC）中,SB505124（500 nM）阻断TGF-β1对F-actin组装的影响,并阻止TGF-β诱导的ROS产生。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (149.08 mM), Sonication is recommended. 1eq. HCl : 33.5 mg/mL (100 mM)
关键字	SB505124 \| SB-505124 \| SB 505124 \| Transforming growth factor beta receptors \| TGF-β Receptor \| Inhibitor \| inhibit
相关产品	Monocrotaline \| Pirfenidone \| Ceritinib \| A 83-01 \| Chromenone 1 \| LY-364947 \| BMP signaling agonist sb4 \| Alectinib hydrochloride \| SB-431542 \| Galunisertib \| Alantolactone \| Hydrochlorothiazide
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 细胞因子抑制剂库 \| 激酶抑制剂库 \| 抗肥胖化合物库 \| TGF-β/Smad靶点化合物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库

SB-505124|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务